Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry of New Jersey Medical School, 185 South Orange Avenue, Newark, New Jersey 07103, USA.
Biochemistry. 2011 Sep 20;50(37):8067-77. doi: 10.1021/bi200815e. Epub 2011 Aug 23.
Earlier, we postulated that Gln91 of human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) stabilizes the side chain of Tyr183 via hydrogen bonding interaction between O(H) of Tyr183 and CO of Q91 [Harris, D., et al. (1998) Biochemistry 37, 9630-9640]. To test this hypothesis, we generated mutant derivatives of Gln91 and analyzed their biochemical properties. The efficiency of reverse transcription was severely impaired by nonconservative substitution of Gln with Ala, while conservative substitution of Gln with Asn resulted in an approximately 70% loss of activity, a value similar to that observed with the Y183F mutation. The loss of polymerase activity from both Q91A and Q91N was significantly improved by a Met to Val substitution at position 184. Curiously, the Q91N mutant exhibited stringency in discriminating between correct and incorrect nucleotides, suggesting its possible interaction with residues influencing the flexibility of the dNTP binding pocket. In contrast, both double mutants, Q91A/M184V and Q91N/M184V, are found to be as error prone as the wild-type enzyme. We propose a model that suggests that subtle structural changes in the region due to mutation at position 91 may influence the stability of the side chain of Tyr183 in the catalytic YMDD motif of the enzyme, thus altering the active site geometry that may interfere in substrate recognition.
早些时候,我们推测人类免疫缺陷病毒 1 型逆转录酶 (HIV-1 RT) 的 Gln91 通过 Tyr183 的 O(H)与 Q91 的 CO 之间的氢键相互作用稳定 Tyr183 的侧链[Harris, D., et al. (1998) Biochemistry 37, 9630-9640]。为了验证这一假设,我们生成了 Gln91 的突变衍生物,并分析了它们的生化特性。用丙氨酸非保守取代 Gln 严重损害了逆转录的效率,而用天冬酰胺保守取代 Gln 导致活性约降低 70%,与 Y183F 突变观察到的活性相似。位置 184 的 Met 到 Val 取代显著改善了 Q91A 和 Q91N 的聚合酶活性丧失。奇怪的是,Q91N 突变体对正确和错误核苷酸具有严格的区分能力,表明其可能与影响 dNTP 结合口袋灵活性的残基相互作用。相比之下,双突变体 Q91A/M184V 和 Q91N/M184V 都被发现与野生型酶一样容易出错。我们提出了一个模型,表明由于位置 91 的突变导致该区域的细微结构变化可能影响酶的催化 YMDD 基序中 Tyr183 侧链的稳定性,从而改变可能干扰底物识别的活性位点几何形状。